Castro-Ruiz Jesús Eduardo, Rojas-Molina Alejandra, Luna-Vázquez Francisco J, Rivero-Cruz Fausto, García-Gasca Teresa, Ibarra-Alvarado César
Laboratorio de Biología Celular y Molecular, Facultad de Ciencias Naturales, Universidad Autónoma de Querétaro, Campus Juriquilla, 76230 Querétaro, Qro., Mexico.
Laboratorio de Investigación Química y Farmacológica de Productos Naturales, Facultad de Ciencias Químicas, Universidad Autónoma de Querétaro, Centro Universitario, 76010 Querétaro, Qro., Mexico.
Int J Mol Sci. 2017 Jan 22;18(1):218. doi: 10.3390/ijms18010218.
roots have been widely used in Mexican traditional medicine to relieve pain, mainly, toothaches. Previous studies have shown that affinin, the major alkamide of these roots, induces potent antinociceptive and anti-inflammatory activities. However, the effect of root extracts and affinin on the cardiovascular system have not been investigated so far. In the present study, we demonstrated that the dichloromethane and ethanolic extracts of roots, and affinin, isolated from these roots, produce a concentration-dependent vasodilation of rat aorta. Affinin-induced vasorelaxation was partly dependent on the presence of endothelium and was significantly blocked in the presence of inhibitors of NO, H₂S, and CO synthesis (N-nitro-l-arginine methyl ester (l-NAME), dl-propargylglycine (PAG), and chromium mesoporphyrin (CrMP), respectively); K⁺ channel blockers (glibenclamide (Gli) and tetraethyl ammonium (TEA)), and guanylate cyclase and cyclooxygenase inhibitors (1-[1,2,4]oxadiazolo[4,3-]quinoxalin-1-one (ODQ) and indomethacin (INDO), respectively). Our results demonstrate, for the first time, that affinin induces vasodilation by mechanisms that involve gasotransmitters, and prostacyclin signaling pathways. These findings indicate that this natural alkamide has therapeutic potential in the treatment of cardiovascular diseases.
这些根在墨西哥传统医学中被广泛用于缓解疼痛，主要是牙痛。先前的研究表明，这些根中的主要酰胺类化合物阿菲宁具有强大的抗伤害感受和抗炎活性。然而，迄今为止，根提取物和阿菲宁对心血管系统的影响尚未得到研究。在本研究中，我们证明了根的二氯甲烷和乙醇提取物以及从这些根中分离出的阿菲宁能使大鼠主动脉产生浓度依赖性血管舒张。阿菲宁诱导的血管舒张部分依赖于内皮的存在，并且在一氧化氮、硫化氢和一氧化碳合成抑制剂（分别为N-硝基-L-精氨酸甲酯（L-NAME）、dl-炔丙基甘氨酸（PAG）和中卟啉铬（CrMP））、钾通道阻滞剂（格列本脲（Gli）和四乙铵（TEA））以及鸟苷酸环化酶和环氧化酶抑制剂（分别为1-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮（ODQ）和吲哚美辛（INDO））存在时被显著阻断。我们的结果首次证明，阿菲宁通过涉及气体递质和前列环素信号通路的机制诱导血管舒张。这些发现表明，这种天然酰胺类化合物在治疗心血管疾病方面具有治疗潜力。
